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盐酸赛拉嗪的药代动力学:一项种间研究。

The pharmacokinetics of xylazine hydrochloride: an interspecific study.

作者信息

Garcia-Villar R, Toutain P L, Alvinerie M, Ruckebusch Y

出版信息

J Vet Pharmacol Ther. 1981 Jun;4(2):87-92. doi: 10.1111/j.1365-2885.1981.tb00715.x.

Abstract

The pharmacokinetic disposition of xylazine hydrochloride is described after both intravenous and intramuscular injection of a single dose, in four domestic species: horse, cattle, sheep and dog, by an original high performance liquid chromatographic technique. Remarkably small interspecific differences are reported. After intravenous administration, systemic half-life (t1/2 beta) ranged between 22 min (sheep) and 50 min (horse) while the distribution phase is transient with half-life (t1/2 alpha) ranging from 1.2 min (cattle) to 5.9 min (horse). The peak level of drug concentration in the plasma is reached after 12-14 min in all the species studied following intramuscular administration. Xylazine bioavailability, as measured by the ratios of the areas under the intravenous and intramuscular plasma concentration versus time curves, ranged from 52% to 90% in dog, 17% to 73% in sheep and 40% to 48% in horse. The low dosage in cattle did not permit calculation. Kinetic data are correlated with clinical data and the origins of interspecific differences are discussed.

摘要

采用一种原创的高效液相色谱技术,在四种家畜(马、牛、羊和狗)单次静脉注射和肌肉注射盐酸赛拉嗪后,描述了其药代动力学特征。报告显示种间差异非常小。静脉给药后,全身半衰期(t1/2β)在22分钟(羊)至50分钟(马)之间,而分布相是短暂的,半衰期(t1/2α)从1.2分钟(牛)至5.9分钟(马)。在所有研究的物种中,肌肉注射后12 - 14分钟达到血浆药物浓度峰值。通过静脉和肌肉血浆浓度与时间曲线下面积之比测量的赛拉嗪生物利用度,在狗中为52%至90%,在羊中为17%至73%,在马中为40%至48%。牛的低剂量不允许进行计算。动力学数据与临床数据相关,并讨论了种间差异的来源。

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